FMK-MEA |
| رقم الكتالوجGC34197 |
FMK-MEA هو مثبط قوي وانتقائي لـ p90 Ribosomal S6 Kinase (RSK).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1414811-15-6
Sample solution is provided at 25 µL, 10mM.
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FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.
FMK-MEA is a water-soluble derivative of fmk. FMK-MEA treatment inhibits RSK2 kinase activity in diverse, highly invasive human cancer cell lines including 212LN, M4e, A549, and SKBR3 cells. Treatment with the RSK-specific inhibitor FMK-MEA significantly attenuates RSK2 activity, as assessed by the phosphorylation levels of Ser-386 and the consequent invasive ability of A549 cells[1].
FMK-MEA treatment (80 mg/kg/day for 16 days by intraperitoneal injection) in highly metastatic M4e cell xenograft nude mice results in a significant attenuation of LN metastasis. FMK-MEA treatment has no effect on the tumor size, and the proliferation rate of the primary tumor[1].
[1]. Li D, et al. The prometastatic ribosomal S6 kinase 2-cAMP response element-binding protein (RSK2-CREB) signaling pathway up-regulates the actin-binding protein fascin-1 to promote tumor metastasis. J Biol Chem. 2013 Nov 8;288(45):32528-38.
Animal experiment: | Mice[1]For FMK-MEA treatment, each of the nude mice (athymic nu/nu, female, 4-6 weeks old) are injected with 0.5×106cells/100 μL of PBS submandibular to the mylohyoid muscle. On day 5 after injection, mice are divided into two groups with similar average weights with each group receiving either FMK-MEA or PBS. Each mouse is administered 80 mg/kg of FMK-MEA daily by intraperitoneal injection from 5 days after the xenograft for 16 days total. The control group receives PBS alone on the same schedule. Tumor growth is recorded. Mice are sacrificed after 16 days post drug treatment[1]. |
References: [1]. Li D, et al. The prometastatic ribosomal S6 kinase 2-cAMP response element-binding protein (RSK2-CREB) signaling pathway up-regulates the actin-binding protein fascin-1 to promote tumor metastasis. J Biol Chem. 2013 Nov 8;288(45):32528-38. | |
| Cas No. | 1414811-15-6 | SDF | |
| Canonical SMILES | FCC(C1=C(C2=CC=C(C)C=C2)C3=C(N)N=CN=C3N1CCCNCCOC)=O | ||
| Formula | C21H26FN5O2 | M.Wt | 399.46 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5034 mL | 12.5169 mL | 25.0338 mL |
| 5 mM | 500.7 μL | 2.5034 mL | 5.0068 mL |
| 10 mM | 250.3 μL | 1.2517 mL | 2.5034 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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